Resminostat is an orally bioavailable inhibitor of histone deacetylase 1 (HDAC1), HDAC3, and HDAC6 (IC50s = 43-72 nM), resulting in hyperacetylation of histone H4 in multiple myeloma cells. It abrogates cell growth and strongly induces apoptosis in multiple myeloma cells (IC50s = 2.5-3 μM). Resminostat displays synergistic effects when combined with melphalan and the proteasome inhibitors bortezomib and S-2209. It dose-dependently inhibits HDAC activity in vivo.
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